Patent · US Expired

Stereospecific production of 6- or 7-carbon-substituted-.beta.-lactams

US4237051A · kind A · utility

18Cited by
9References
11Claims
0Family size

Assignee

Inventor

Key dates

Filing dateApr 19, 1979
Grant dateDec 2, 1980
Priority date
Expiry dateApr 19, 1999

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D499/00
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Reaction of 6- or 7-diazo-.beta.-lactams with allylic halides in the presence of a catalytic amount of metallic copper or a copper salt affords 6- or 7-carbon-substituted-.beta.-lactams with the desired stereochemical configuration at the 6- or 7-position. Subsequent reduction with a trialkyl stannane affords useful intermediates for further syntheses affording 6- or 7-carbon-substituted-.beta.-lactams. The present invention relates to a process for the production of 6- or 7-carbon-substituted-.beta.-lactams having the desired stereochemical configuration at the 6- or 7-position. More particularly, this invention provides a process for the preparation of a .beta.-lactam of the formula ##STR1## wherein R.sub.1 is cyano or COOR.sub.2 wherein R.sub.2 is a readily removable ester-forming moiety, hydrogen or an alkali-metal cation; PA0 R.sub.3 and R.sub.4 are independently hydrogen, lower alkyl, aryl or aralkyl; PA0 Z is a group of the formula ##STR2## wherein R.sub.5 is hydrogen, lower alkyl or aralkyl; and the dotted line indicates the optional presence of a double bond; which comprises PA1 (1) reacting a diazo-.beta.-lactam of the formula ##STR3## wherein Y is a sulfur or an oxygenat…

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.